High-stability ampelopsis grossedentata extract polymer micelle composition

Abstract

The invention provides a polymer micelle composition. The polymer micelle composition is prepared from ampelopsis grossedentata extract or dihydromyricetin, an amphiphilic polymer capable of forming a polymer micelle; and an antioxidant. The invention also provides a method for preparing the polymer micelle composition. The invention also relates to application of the polymer micelle composition in preparation of medicines or cosmetics. The invention further relates to medicines or cosmetics containing the polymer micelle composition.

Description

Technical Field

[0001] The present invention relates to a rattan tea extract polymer micelle composition with high stability. The polymer micelle composition of the present invention comprises a rattan tea extract or dihydromyricetin; an amphiphilic polymer capable of forming polymer micelles; and an antioxidant. The present invention also relates to a method for preparing the composition, use of the composition in preparing a medicine or cosmetic, and a medicine or cosmetic containing the composition. Background Art

[0002] Ampelopsis grossedentata, belonging to the family Vitaceae, is widely distributed in Hunan, Guangdong, Guangxi, Fujian and other places in my country. Ampelopsis grossedentata has a long history of being used as both a medicinal tea and a tea in China. For example, the Shennong's Herbal Classic states that "tea tastes bitter, and drinking it can improve thinking, reduce lying, lighten the body, and improve eyesight". Ampelopsis chaffanjoni, Ampelopsis megalophylla and Ampelopsis cantoniensis can also be used as raw materials for Ampelopsis chaffanjoni, Ampelopsis megalophylla and Ampelopsis cantoniensis. Modern research shows that the main active ingredient of Ampelopsis chaffanjoni is dihydromyricetin, which can reach 30%, and has multiple physiological activities such as scavenging ROS, anti-inflammatory, antibacterial, inhibiting tyrosinase, inhibiting melanin, inhibiting sebaceous gland cell oil, and promoting collagen genes. Therefore, Ampelopsis grossedentata extract is very suitable as an active raw material for the preparation of functional cosmetics such as whitening, anti-oxidation, anti-aging, and anti-acne. However, the solubility of dihydromyricetin in the extract of Rhizoma Coptidis in water at 25°C is only 0.2 mg / mL. [1] , the half-life at 45°C is only 17.9 days [2] The tea soup of rattan tea will change color and precipitate when stored at high temperature. [3] The above properties of rattan tea extract severely limit and affect the effective addition, efficacy activity and sensory experience of rattan tea extract in cosmetic formulas.

[0003] Regarding the water solubility and stability of rattan tea extract or dihydromyricetin, the basic situation of existing technical means is as follows:

[0004] 1. CN 118593394 A discloses a rattan tea complex and its preparation method and cosmetics, wherein the rattan tea complex uses dipropylene glycol, glycerol and betaine as solubilizing carriers, the rattan tea extract content is 10%, and can be diluted with water in any proportion. However, the introduction of betaine will greatly increase the pH of the system, thereby accelerating the discoloration and oxidation of the rattan tea extract.

[0005] 2. Chen Yuqiong et al. [3]The effects of β-cyclodextrin (β-CD) and ascorbic acid (also known as vitamin C (VC)) on the quality stability of rattan tea beverages were studied. It was found that the addition of vitamin C is beneficial to the preservation of tea flavonoids, as well as the color quality and the reduction of precipitation formation; β-CD has a significant effect on reducing tea precipitation and crystallization, but has no significant effect on protecting tea flavonoids and color. However, β-CD has poor water solubility and limited solubilization effect, and is not suitable for cosmetic applications; vitamin C itself is easy to change color and has poor color protection effect.

[0006] In the above disclosed invention method, although the water solubility and stability of dihydromyricetin are improved to varying degrees, there are still many deficiencies in the application of cosmetics, such as but not limited to the following deficiencies:

[0007] (1) The solubilization, color protection and stabilization effects on rattan tea extract are limited and are not suitable for use as cosmetics;

[0008] (2) The preparation process is complicated, the amount of auxiliary materials used is high, and the irritation is high, requiring the use of certain irritating organic solvents to aid dissolution.

[0009] Therefore, there is an urgent need for a rattan tea extract composition that can improve the water solubility of rattan tea extract or dihydromyricetin in cosmetic formulas, stabilize the content of dihydromyricetin therein, prevent dihydromyricetin from being oxidized, and at the same time delay the discoloration of the rattan tea extract in the formula, and has a simple preparation process, is non-irritating, and does not require the use of organic solvents. Summary of the invention

[0010] The present invention relates to a polymer micelle composition, which comprises a rattan tea extract or dihydromyricetin as an active ingredient, an amphiphilic polymer capable of forming polymer micelles, and an antioxidant. The polymer micelle composition has the following advantages:

[0011] (1) The insoluble dihydromyricetin is encapsulated by forming polymer micelles with amphiphilic polymers, thereby improving the solubility and stability of the rattan tea extract or dihydromyricetin in the preparation. Compared with traditional small molecule surfactant micelles, the polymer micelles have lower critical micelle concentration (CMC) values ​​and irritation, better stability and biocompatibility, and are easy to dry into powder, and can be added to cosmetic formulas at high concentrations;

[0012] (2) Through rationally designed antioxidants, the oxidation deterioration of the main active ingredient dihydromyricetin can be reduced, the main active ingredient can be stabilized, and the undesirable color changes caused by oxidation in the cosmetic composition can be reduced;

[0013] (3) The present invention combines polymer micelle technology with rationally designed antioxidants, and has better effects in solubilizing and stabilizing the rattan tea extract through physical and chemical dual stabilization effects;

[0014] (4) The rattan tea extract polymer micelles provided by the present invention retain the characteristic aroma and efficacy of rattan tea, have a clear and transparent appearance, can be diluted in any proportion, and are suitable for use as a cosmetic functional raw material.

[0015] The first aspect of the present invention relates to a polymer micelle composition comprising the following components:

[0016] (a) rattan tea extract or dihydromyricetin;

[0017] (b) an amphiphilic polymer capable of forming polymer micelles;

[0018] (c) Antioxidants.

[0019] The second aspect of the present invention relates to a method for preparing the polymer micelle composition according to the first aspect of the present invention, the method comprising the following steps:

[0020] (1) loading component (a) onto an amphiphilic polymer of component (b) to form component (a) fully or partially encapsulated in polymer micelles;

[0021] (2) Add antioxidants,

[0022] Wherein step (1) and step (2) can be carried out simultaneously or sequentially; wherein the ratio and content of each component are as defined in any one of claims 1 to 9; optionally, water and / or an ingredient having an antibacterial effect are added simultaneously in step (1).

[0023] The third aspect of the present invention relates to use of the polymer micelle composition according to the first aspect of the present invention in the preparation of medicines / cosmetics.

[0024] The fourth aspect of the present invention relates to a medicine or cosmetic, comprising the polymer micelle composition according to the first aspect of the present invention, wherein the micelle composition accounts for 1% to 60% by weight of the medicine or cosmetic. BRIEF DESCRIPTION OF THE DRAWINGS

[0025] Figure 1 The following are appearance diagrams of samples of Examples 1-5 and Comparative Examples 1-8 according to the present invention before storage at 60°C.

[0026] Figure 2 The following are appearance diagrams of samples of Examples 1-5 and Comparative Examples 1-8 according to the present invention after being stored at 60° C. for 7 days.

[0027] Figure 3 The following are appearance diagrams of samples of Examples 1-5 and Comparative Examples 1-8 according to the present invention after being stored at 60° C. for 14 days. DETAILED DESCRIPTION OF THE INVENTION

[0029] definition

[0030] As used herein, the terms "s", "min" and "h" stand for "seconds", "minutes" and "hours", respectively.

[0031] As used herein, the term "comprising", which is synonymous with "including", "containing" or "characterized by", is inclusive or open-ended and does not exclude additional, undescribed elements or method steps. However, in the text, each time "comprising" is mentioned, it is intended to cover the alternative embodiments of "consisting essentially of" and "consisting of", wherein "consisting of" excludes any elements or steps not specified, and "consisting essentially of" allows the inclusion of other elements or steps not described that do not materially affect the essential or basic characteristics and novel characteristics of the composition or method in question.

[0032] The term "about" as used herein refers to ±10%, more preferably ±5%, and most preferably ±2% of the value modified by the term, so that a person skilled in the art can clearly determine the scope of the term "about" based on the modified value.

[0033] As defined herein, "amphiphilic polymer capable of forming polymer micelles" refers to a macromolecular polymer whose hydrophilic region and hydrophobic region are connected by covalent bonds. When the concentration of such an amphiphilic polymer containing two incompatible parts with different solubility in water is greater than its critical micelle concentration (CMC), it can spontaneously form a thermodynamically stable system having a hydrophilic outer shell and a hydrophobic inner core, i.e., a micelle.

[0034] As defined herein, "Poloxamer 407" is a nonionic surfactant, and its trade names include Pluronic F127, Pluracare TM F127 Prill Surfactant, P 407, etc., its molecular weight is 12600g / mol, CAS number is 9003-11-6, it is a block copolymer, a synthetic copolymer of ethylene oxide and propylene oxide, the chemical structure is as follows:

[0035]

[0036] Where a and b have the following values:

[0037] a b 98-101 56 .

[0038] Polymer micelle composition

[0039] The first aspect of the present invention relates to a polymer micelle composition comprising the following components:

[0040] (a) rattan tea extract or dihydromyricetin;

[0041] (b) an amphiphilic polymer capable of forming polymer micelles;

[0042] (c) Antioxidants.

[0043] In some embodiments, the amphiphilic polymer is a cosmetically acceptable amphiphilic polymer. In some embodiments, the amphiphilic polymer is a non-toxic, non-irritating amphiphilic polymer.

[0044] In some embodiments, the amphiphilic polymer is selected from poloxamer 407, poloxamer 188, poloxamer 184, vitamin E polyethylene glycol succinate, or a combination thereof. In some embodiments, the amphiphilic polymer is poloxamer 407.

[0045] In the present invention, the specific model of poloxamer 407 used is Pluracare TM F127 PrillSurfactant, at Pluracare TM In addition to poloxamer 407 as the main active ingredient, F127 Prill Surfactant also generally includes a small amount of butylated hydroxytoluene. In some embodiments, the poloxamer 407 is Pluracare TM F127 Prill Surfactant.

[0046] In some embodiments, the polymer micelle composition optionally further comprises butylated hydroxytoluene.

[0047] In some embodiments, the antioxidant is a cosmetically acceptable antioxidant. In some embodiments, the antioxidant is a non-toxic, non-irritating antioxidant.

[0048] In some embodiments, the antioxidant can reduce the discoloration of the vine tea extract or dihydromyricetin after long-term storage. In some embodiments, the antioxidant can reduce the discoloration of the vine tea extract or dihydromyricetin after long-term storage at room temperature. In some embodiments, the antioxidant can reduce the discoloration of the vine tea extract or dihydromyricetin after long-term storage at a temperature of 40-90°C.

[0049] In some embodiments, the antioxidant can reduce the oxidative deterioration of the vine tea extract or dihydromyricetin after long-term storage. In some embodiments, the antioxidant can reduce the oxidative deterioration of the vine tea extract or dihydromyricetin after long-term storage at room temperature. In some embodiments, the antioxidant can reduce the oxidative deterioration of the vine tea extract or dihydromyricetin after long-term storage at a temperature of 40-90°C.

[0050] In some embodiments, the antioxidant is selected from one, a combination of two or more of vitamin C, sodium pyrosulfite, ascorbyl glucoside, vitamin C ethyl ether, gallic acid, propyl gallate, tea polyphenols, butylated hydroxytoluene and epigallocatechin gallate. In some embodiments, the antioxidant is a combination of sodium pyrosulfite and one or more selected from vitamin C, ascorbyl glucoside, vitamin C ethyl ether, gallic acid, propyl gallate, tea polyphenols, butylated hydroxytoluene and epigallocatechin gallate. In some embodiments, the antioxidant is a combination of sodium pyrosulfite and vitamin C.

[0051] In some embodiments, the polymer micelle composition optionally further comprises water and / or an ingredient having a bacteriostatic effect.

[0052] In some embodiments, the antibacterial component is selected from butylene glycol, hexylene glycol, chloranone, propylene glycol, pentylene glycol, octanediol, phenoxyethanol, ethylhexylglycerol or a combination thereof. In some embodiments, the antibacterial component is a combination of butylene glycol, hexylene glycol and chloranone.

[0053] In some embodiments, the weight ratio of component (a) to component (b) is 1:1 to 1:40. In some embodiments, the weight ratio of component (a) to component (b) is 1:1 to 1:2, 1:2 to 1:3, 1:3 to 1:4, 1:4 to 1:5, 1:5 to 1:6, 1:6 to 1:7, 1:7 to 1:8, 1:8 to 1:9, 1:9 to 1:10, 1:10 to 1:11, 1:11 to 1:12, 1:12 to 1:13, 1:13 to 1:14, 1:14 to 1:15, 1:15 to 1:16, 1:16 to 1:17, 1:17 to 1:18, 1:18 to 1:19, 1:19 to 1:20, 1:20 to 1:21. 1:37 to 1:38, 1:38 to 1:39, 1:39 to 1:40, or any combination of these ranges. In some embodiments, the weight ratio of component (a) to component (b) is 1:2 to 1:20.

[0054] In some embodiments, the weight ratio of component (a) to component (c) is 1:20 to 100: 1. In some embodiments, the weight ratio of component (a) to component (c) is 1:20 to 1:15, 1:15 to 1:10, 1:10 to 1:5, 1:5 to 5:12, 5:12 to 1:1, 1:1 to 5:1, 5:1 to 10:1, 10:1 to 15:1, 15:1 to 20:1, 20:1 to 25:1, 25:1 to 30:1, 30:1 to 35:1, 35:1 to 30 ... 1 to 50:1, 50:1 to 55:1, 55:1 to 60:1, 60:1 to 65:1, 65:1 to 70:1, 70:1 to 75:1, 75:1 to 80:1, 80:1 to 85:1, 85:1 to 90:1, 90:1 to 95:1, 95:1 to 100:1, or any combination of these ranges. In some embodiments, the weight ratio of component (a) to component (c) is 5:12 to 25:1.

[0055] In some embodiments, when component (c) is a combination of vitamin C and sodium metabisulfite, the weight ratio of vitamin C to sodium metabisulfite is 1: 10 to 50: 1. In certain embodiments, when component (c) is a combination of vitamin C and sodium metabisulfite, the weight ratio of vitamin C to sodium metabisulfite is 1: 10 to 1: 5, 1: 5 to 1: 1, 1: 1 to 2: 1, 2: 1 to 3: 1, 3: 1 to 4: 1, 4: 1 to 5: 1, 5: 1 to 10: 1, 10: 1 to 15: 1, 15: 1 to 20: 1, 20: 1 to 25: 1, 25: 1 to 30: 1, 30: 1 to 35: 1, 35: 1 to 40: 1, 40: 1 to 45: 1, 45: 1 to 50: 1, or any combination of these ranges. In certain embodiments, when component (c) is a combination of vitamin C and sodium metabisulfite, the weight ratio of vitamin C to sodium metabisulfite is 1:1 to 5:1.

[0056] In some embodiments, the concentration of the component (a) is 0.01% to 10% by weight. In certain embodiments, the concentration of the component (a) is 0.01% to 0.05%, 0.05% to 0.1%, 0.1% to 0.5%, 0.5% to 1%, 1% to 1.5%, 1.5% to 2%, 2% to 2.5%, 2.5% to 3%, 3% to 3.5%, 3.5% to 4%, 4% to 4.5%, 4.5% to 5%, 5% to 6%, 6% to 7%, 7% to 8%, 8% to 9%, 9% to 10% or any combination of these ranges by weight. In certain embodiments, the concentration of the component (a) is 0.1% to 5% by weight.

[0057] In some embodiments, the concentration of the component (b) is greater than its critical micelle concentration and is 0.1% to 50% by weight. In some embodiments, the concentration of the component (b) is greater than its critical micelle concentration and is 0.1% to 0.5%, 0.5% to 1%, 1% to 2%, 2% to 3%, 3% to 4%, 4% to 5%, 5% to 6%, 6% to 7%, 7% to 8%, 8% to 9%, 9% to 10%, 10% to 15%, 15% to 20%, 20% to 25%, 25% to 30%, 30% to 35%, 35% to 40%, 40% to 45%, 45% to 50% or any combination of these ranges by weight. In some embodiments, the concentration of the component (b) is greater than its critical micelle concentration and is 1% to 10% by weight.

[0058] In some embodiments, the concentration of component (c) is 0.001% to 10% by weight. In some embodiments, the concentration of component (c) is 0.001% to 0.005%, 0.005% to 0.01%, 0.01% to 0.015%, 0.015% to 0.02%, 0.02% to 0.03%, 0.03% to 0.04%, 0.04% to 0.05%, 0.05% to 0.06%, 0.06% to 0.07%, 0.07% to 0.08%, 0.08% to 0.09%, 0.09% to 0.1%, 0.1% to 0. %, 0.2% to 0.3%, 0.3% to 0.4%, 0.4% to 0.5%, 0.5% to 0.6%, 0.6% to 0.7%, 0.7% to 0.8%, 0.8% to 0.9%, 0.9% to 1.0%, 1.0% to 1.1%, 1.1% to 1.2%, 1.2% to 1.5%, 1.5% to 2%, 2% to 3%, 3% to 4%, 4% to 5%, 5% to 6%, 6% to 7%, 7% to 8%, 8% to 9%, 9% to 10%, or any combination of these ranges. In some embodiments, the concentration of component (c) is 0.02% to 1.2% by weight.

[0059] In some embodiments, when component (c) is a combination of vitamin C and sodium metabisulfite, the concentration of vitamin C is 0.001% to 10% by weight. In some embodiments, when component (c) is a combination of vitamin C and sodium metabisulfite, the concentration of vitamin C is 0.001% to 0.005%, 0.005% to 0.01%, 0.01% to 0.05%, 0.05% to 0.1%, 0.1% to 0.2%, 0.2% to 0.3%, 0.3% to 0.4%, 0.4% to 0.5%, 0.5% to 0.6%, 0.6% to 0.7%, 0.7% to 0.8%, 0.8% to 0.9%, 0.9% to 1%, 1% to 2%, 2% to 3%, 3% to 4%, 4% to 5%, 5% to 6%, 6% to 7%, 7% to 8%, 8% to 9%, 9% to 10%, or any combination of these ranges by weight. In some embodiments, when component (c) is a combination of vitamin C and sodium metabisulfite, the concentration of vitamin C is 0.01% to 1% by weight.

[0060] In some embodiments, when component (c) is a combination of vitamin C and sodium metabisulfite, the concentration of sodium metabisulfite is 0.001% to 10% by weight. In some embodiments, when component (c) is a combination of vitamin C and sodium metabisulfite, the concentration of sodium metabisulfite is 0.001% to 0.005%, 0.005% to 0.01%, 0.01% to 0.05%, 0.05% to 0.1%, 0.1% to 0.2%, 0.2% to 0.3%, 0.3% to 0.4%, 0.4% to 0.5%, 0.5% to 0.6%, 0.6% to 0.7%, 0.7% to 0.8%, 0.8% to 0.9%, 0.9% to 1%, 1% to 2%, 2% to 3%, 3% to 4%, 4% to 5%, 5% to 6%, 6% to 7%, 7% to 8%, 8% to 9%, 9% to 10%, or any combination of these ranges by weight. In some embodiments, when component (c) is a combination of vitamin C and sodium metabisulfite, the concentration of sodium metabisulfite is 0.01% to 0.2% by weight.

[0061] In some embodiments, when the ingredient having an antibacterial effect is a combination of butanediol, hexanediol and cinnamaldehyde, the weight ratio of butanediol to hexanediol is 1:1 to 20:1. In some embodiments, when the ingredient having an antibacterial effect is a combination of butanediol, hexanediol and cinnamone, the weight ratio of butanediol to hexanediol is 1:1 to 2:1, 2:1 to 3:1, 3:1 to 4:1, 4:1 to 5:1, 5:1 to 6:1, 6:1 to 7:1, 7:1 to 8:1, 8:1 to 9:1, 9:1 to 10:1, 10:1 to 11:1, 11:1 to 12:1, 12:1 to 13:1, 13:1 to 14:1, 14:1 to 15:1, 15:1 to 16:1, 16:1 to 17:1, 17:1 to 18:1, 18:1 to 19:1, 19:1 to 20:1, or any combination of these ranges. In some embodiments, when the ingredient having an antibacterial effect is a combination of butanediol, hexanediol and cinnamaldehyde, the weight ratio of butanediol to hexanediol is 10:1.

[0062] In some embodiments, when the ingredient having an antibacterial effect is a combination of butanediol, hexanediol and cinnamaldehyde, the weight ratio of butanediol to cinnamaldehyde is 1:1 to 20:1. In some embodiments, when the ingredient with antibacterial effect is a combination of butanediol, hexanediol and cinnamaldehyde, the weight ratio of butanediol to cinnamaldehyde is 1:1 to 2:1, 2:1 to 3:1, 3:1 to 4:1, 4:1 to 5:1, 5:1 to 6:1, 6:1 to 7:1, 7:1 to 8:1, 8:1 to 9:1, 9:1 to 10:1, 10:1 to 11:1, 11:1 to 12:1, 12:1 to 13:1, 13:1 to 14:1, 14:1 to 15:1, 15:1 to 16:1, 16:1 to 17:1, 17:1 to 18:1, 18:1 to 19:1, 19:1 to 20:1 or any combination of these ranges. In some embodiments, when the ingredient having an antibacterial effect is a combination of butanediol, hexanediol and cinnamaldehyde, the weight ratio of butanediol to cinnamaldehyde is 10:1.

[0063] In some embodiments, when the antibacterial ingredient is a combination of butanediol, hexanediol and fenvalerate, the weight of butanediol in the composition accounts for 1%-20% of the weight of the preservative water composed of butanediol, hexanediol, fenvalerate and water in the composition. In some embodiments, when the ingredient with antibacterial effect is a combination of butanediol, hexanediol and cinnamaldehyde, the weight of butanediol in the composition accounts for 1%-2%, 2%-3%, 3%-4%, 4%-5%, 5%-6%, 6%-7%, 7%-8%, 8%-9%, 9%-10%, 10%-11%, 11%-12%, 12%-13%, 13%-14%, 14%-15%, 15%-16%, 16%-17%, 17%-18%, 18%-19%, 19%-20% or any combination of these ranges of the weight of the preservative water composed of butanediol, hexanediol, cinnamaldehyde and water in the composition. In some embodiments, when the antibacterial ingredient is a combination of butanediol, hexanediol and fenvalerate, the weight of butanediol in the composition accounts for 5% of the weight of the preservative water composed of butanediol, hexanediol, fenvalerate and water in the composition.

[0064] In some embodiments, when the antibacterial component is a combination of butanediol, hexanediol and cinnamic acid, the weight of hexanediol in the composition accounts for 0.1%-5% of the weight of the preservative water composed of butanediol, hexanediol, cinnamic acid and water in the composition. In some embodiments, when the antibacterial component is a combination of butanediol, hexanediol and cinnamic acid, the weight of hexanediol in the composition accounts for 0.1%-0.2%, 0.2%-0.3%, 0.3%-0.4%, 0.4%-0.5%, 0.5%-0.6%, 0.6%-0.7%, 0.7%-0.8%, 0.8%-0.9%, 0.9%-1%, 1%-2%, 2%-3%, 3%-4%, 4%-5% or any combination of these ranges of the weight of the preservative water composed of butanediol, hexanediol, cinnamic acid and water in the composition. In some embodiments, when the antibacterial ingredient is a combination of butanediol, hexanediol and chloranone, the weight of hexanediol in the composition accounts for 0.5% of the weight of the preservative water composed of butanediol, hexanediol, chloranone and water in the composition.

[0065] In some embodiments, when the antibacterial component is a combination of butanediol, hexanediol and xinxian ketone, the weight of xinxian ketone in the composition accounts for 0.1%-5% of the weight of the preservative water composed of butanediol, hexanediol, xinxian ketone and water in the composition. In some embodiments, when the antibacterial component is a combination of butanediol, hexanediol and xinxian ketone, the weight of xinxian ketone in the composition accounts for 0.1%-0.2%, 0.2%-0.3%, 0.3%-0.4%, 0.4%-0.5%, 0.5%-0.6%, 0.6%-0.7%, 0.7%-0.8%, 0.8%-0.9%, 0.9%-1%, 1%-2%, 2%-3%, 3%-4%, 4%-5% or any combination of these ranges of the weight of the preservative water composed of butanediol, hexanediol, xinxian ketone and water in the composition. In some embodiments, when the ingredient with antibacterial effect is a combination of butanediol, hexanediol and fenvalerate, the weight of fenvalerate in the composition accounts for 0.5% of the weight of the preservative water composed of butanediol, hexanediol, fenvalerate and water in the composition.

[0066] In some embodiments, the rattan tea is a rattan tea derived from a raw material selected from Ampelopsis Grossedentata, Ampelopsis chaffanjoni, Ampelopsis megalophylla and Ampelopsis cantoniensis or a combination thereof.

[0067] In some embodiments, the rattan tea extract is an extract obtained by extracting from rattan tea using a suitable solvent. In some embodiments, the suitable solvent is selected from water, methanol, ethanol, n-butanol, ethyl acetate, propylene glycol, butylene glycol or a combination thereof. In some embodiments, the suitable solvent is water. In some embodiments, the rattan tea extract includes any rattan tea extract known in the prior art.

[0068] In some embodiments, the extract of Ampelopsis ulmoides L. is obtained by a method comprising the following steps:

[0069] (1) extracting the rattan tea with a suitable solvent under heating conditions for 1 to 5 times under reflux;

[0070] (2) Refrigerate overnight and discard the supernatant;

[0071] (3) dissolving the precipitate with 2-5 times (preferably 3 times) the weight of 60%-100% (preferably 95%) ethanol, and filtering to obtain a supernatant; and

[0072] (4) Concentrating and drying to obtain rattan tea extract.

[0073] In some embodiments, the suitable solvent is selected from water, methanol, ethanol, n-butanol, ethyl acetate, propylene glycol, butylene glycol or a combination thereof. In some embodiments, the suitable solvent is water.

[0074] In some embodiments, the content of dihydromyricetin in the vine tea extract is 30% to 99% by weight. In some embodiments, the content of dihydromyricetin in the vine tea extract is 30% to 35%, 35% to 40%, 40% to 45%, 45% to 50%, 50% to 55%, 55% to 60%, 60% to 65%, 65% to 70%, 70% to 75%, 75% to 80%, 80% to 85%, 85% to 90%, 90% to 95%, 95% to 99% or any combination of these ranges by weight. In some embodiments, the content of dihydromyricetin in the vine tea extract is 60% to 75% by weight.

[0075] In some embodiments, the composition does not contain an irritating solvent. In some embodiments, the composition does not contain an irritating solvent selected from methanol, ethanol, chloroform, or a combination thereof. In some embodiments, the composition does not contain methanol. In some embodiments, the composition does not contain ethanol. In some embodiments, the composition does not contain chloroform.

[0076] In some embodiments, the poorly soluble components in the rattan tea extract (including but not limited to dihydromyricetin) are all or partially encapsulated in the micelle core formed by an amphiphilic polymer. In some embodiments, the poorly soluble components in the rattan tea extract (including but not limited to dihydromyricetin) are all or partially encapsulated in the micelle core formed by an amphiphilic polymer, and the encapsulation rate is 50% to 100%. In some embodiments, the poorly soluble components in the rattan tea extract (including but not limited to dihydromyricetin) are all or partially encapsulated in the micelle core formed by an amphiphilic polymer, and the encapsulation rate is 50% to 55%, 55% to 60%, 60% to 65%, 65% to 70%, 70% to 75%, 75% to 80%, 80% to 85%, 85% to 90%, 90% to 95% or 95% to 100%. In some embodiments, the poorly soluble components in the rattan tea extract (including but not limited to dihydromyricetin) are fully or partially encapsulated in the micelle core formed by the amphiphilic polymer, and the encapsulation rate is 50% to 90%.

[0077] In some embodiments, dihydromyricetin is encapsulated in whole or in part in the micelle core formed by an amphiphilic polymer. In some embodiments, dihydromyricetin is encapsulated in whole or in part in the micelle core formed by an amphiphilic polymer, and the encapsulation efficiency is 50% to 100%. In some embodiments, dihydromyricetin is encapsulated in whole or in part in the micelle core formed by an amphiphilic polymer, and the encapsulation efficiency is 50% to 55%, 55% to 60%, 60% to 65%, 65% to 70%, 70% to 75%, 75% to 80%, 80% to 85%, 85% to 90%, 90% to 95% or 95% to 100%. In some embodiments, dihydromyricetin is encapsulated in whole or in part in the micelle core formed by an amphiphilic polymer, and the encapsulation efficiency is 50% to 90%.

[0078] In some embodiments, the polymer micelle composition is stored at room temperature for 4-30 days without precipitation. In some embodiments, the polymer micelle composition is stored at room temperature for 4-5, 5-6, 6-7, 7-8, 8-9, 9-10, 10-15, 15-20, 20-25 or 25-30 days without precipitation. In some embodiments, the polymer micelle composition is stored at room temperature for 4 days without precipitation.

[0079] In some embodiments, the polymer micelle composition has little color deepening after being stored at 30°C-80°C for 5-30 days. In some embodiments, the polymer micelle composition has little color deepening after being stored at 30°C-80°C for 7-14 days. In some embodiments, the polymer micelle composition has little color deepening after being stored at 50°C-70°C for 5-30 days. In some embodiments, the polymer micelle composition has little color deepening after being stored at 50°C-70°C for 7-14 days. In some embodiments, the polymer micelle composition has little color deepening after being stored at 60°C for 5-30 days. In some embodiments, the polymer micelle composition has little color deepening after being stored at 60°C for 7-14 days.

[0080] In some embodiments, after the polymer micelle composition is stored at 30°C-80°C for 5-30 days, the retention rate of dihydromyricetin can be maintained at 95%-100%. In some embodiments, after the polymer micelle composition is stored at 50°C-70°C for 5-30 days, the retention rate of dihydromyricetin can be maintained at 95%-100%. In some embodiments, after the polymer micelle composition is stored at 60°C for 5-30 days, the retention rate of dihydromyricetin can be maintained at 95%-100%. In some embodiments, after the polymer micelle composition is stored at 30°C-80°C for 7-14 days, the retention rate of dihydromyricetin can be maintained at 95%-100%. In some embodiments, after the polymer micelle composition is stored at 50°C-70°C for 7-14 days, the retention rate of dihydromyricetin can be maintained at 95%-100%. In some embodiments, after the polymer micelle composition is stored at 60° C. for 7-14 days, the retention rate of dihydromyricetin can be maintained at 95%-100%.

[0081] Preparation method

[0082] The second aspect of the present invention relates to a method for preparing the polymer micelle composition according to the first aspect of the present invention, the method comprising the following steps:

[0083] (1) loading component (a) onto an amphiphilic polymer of component (b) to form component (a) fully or partially encapsulated in polymer micelles;

[0084] (2) Add antioxidants,

[0085] Wherein step (1) and step (2) can be carried out simultaneously or sequentially; wherein the ratio and content of each component are as defined in the "Polymer micelle composition" section of the detailed description of the invention; optionally, water and / or an ingredient with antibacterial effect are added simultaneously in step (1).

[0086] In some embodiments, step (1) is performed first and then step (2), and step (1) is performed at a temperature of 60-90°C, preferably 75-85°C, and step (2) is performed at room temperature.

[0087] In some embodiments, step (1) comprises stirring component (a), component (b) and optional water and / or an ingredient having an antibacterial effect at a temperature of 60-90° C., preferably 75-85° C.; and step (2) comprises adding an antioxidant after cooling the solution obtained in step (1) to room temperature.

[0088] In some embodiments, the method further comprises the step of concentrating. In some embodiments, the method further comprises the step of concentrating and drying. In some embodiments, the method further comprises the step of concentrating and freeze drying. In some embodiments, the method further comprises the step of concentrating and vacuum drying. In some embodiments, the method further comprises the step of freeze drying. In some embodiments, the method further comprises the step of vacuum drying.

[0089] Use of the composition of the present invention for preparing medicine or cosmetics

[0090] The third aspect of the present invention relates to use of the polymer micelle composition according to the first aspect of the present invention in the preparation of medicines / cosmetics.

[0091] In some embodiments, the medicine / cosmetic has anti-inflammatory, antioxidant, whitening, oil-control, anti-aging, antibacterial and / or anti-acne effects.

[0092] Medicines and cosmetics

[0093] The fourth aspect of the present invention relates to a medicine or cosmetic, comprising the polymer micelle composition according to the first aspect of the present invention, wherein the micelle composition accounts for 1% to 60% by weight of the medicine or cosmetic.

[0094] In some embodiments, the composition comprises 1%-5%, 5%-10%, 10%-15%, 15%-20%, 20%-25%, 25%-30%, 30%-35%, 35%-40%, 40%-45%, 45%-50%, 50%-55%, 55%-60% or any combination of these ranges by weight of the drug or cosmetic.

[0095] In some embodiments, the medicine or cosmetics are used for skin care. In some embodiments, the medicine and cosmetics are used for skin anti-inflammatory, anti-oxidation, whitening, oil control, anti-aging, antibacterial and / or acne removal. In some embodiments, the medicine and cosmetics include the composition according to any one of the first to fourth aspects of the present invention and one or more pharmaceutically or cosmetically acceptable carriers, diluents or excipients. In some embodiments, the medicine and cosmetics are creams, emulsions, pastes, ointments, facial masks, gels, lotions or essences. In some embodiments, the medicine and cosmetics of the present invention may also contain one or more other ingredients, such as plant extracts, nutritional additives, surfactants, flavors and fragrances, pigments, preservatives, antioxidants, moisturizers, ultraviolet absorbers, astringents, penetration aids, pH regulators, etc. Those skilled in the art can make a choice according to their common sense and specific needs.

[0096] In some embodiments, the medicine or cosmetic further comprises one or more other cosmetic active ingredients, such as but not limited to moisturizers, keratin repair agents, oil control agents, oil repellent agents, hydrating agents, anti-allergic agents, anti-aging and anti-wrinkle agents, etc. DETAILED DESCRIPTION

[0097] The present invention can be implemented through the following embodiments, but the present invention is not limited thereto.

[0098] The instruments and equipment used in the embodiments of the present invention are all conventional instruments and equipment in the field and can be replaced by instruments and equipment that meet the corresponding standards.

[0099] The Chinese herbal medicine raw materials used in the embodiments of the present invention are all commercially available unless otherwise specified, and the reagents used in the embodiments of the present invention are all commercially available analytically pure chemical reagents unless otherwise specified.

[0100] The raw materials and instruments and equipment mentioned in the present invention are all commonly used raw materials and instruments and equipment in the field, which are only examples and are not intended to limit the scope of protection of the present invention. Those skilled in the art can select equivalent raw materials and related instruments and equipment based on the disclosure of the present invention.

[0101] Experimental materials, equipment and statistical analysis methods

[0102] Experimental reagents: Pluracare TMF127 Prill Surfactant was purchased from BASF (China) Co., Ltd.; SOLUBILISANT LRI was purchased from Senxin Flavors & Colors Technology (China) Co., Ltd.; 1,3-Butanediol was purchased from Shandong Haike Chemical Group; SymSave H and Hydrolite 6-hexanediol were purchased from Dezhixin Flavors & Fragrances (Nantong) Co., Ltd.; ascorbic acid (vitamin C), sodium metabisulfite, and hydroxypropyl-β-cyclodextrin (HP-β-CD) were purchased from the General-reagent brand of Shanghai Titan Technology Co., Ltd.

[0103] Experimental equipment: (1) Electric heating jacket, ZNHW-II from Gongyi Yuhua Instrument Co., Ltd.; (2) Rotary evaporator, EYELA Tokyo Rikakigi Co., Ltd. N-1100; (3) Vacuum drying oven, VO-50D from Shanghai Yuanhuai Intelligent Technology Co., Ltd.; (4) Electric constant temperature water bath, HWS-24 from Shanghai Yiheng Scientific Instrument Co., Ltd.

[0104] Example

[0105] Preparation Example

[0106] Example 1

[0107] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0108] Based on the weight percentage (the same below), 0.5% of rattan tea extract, Pluracare TM F127 PrillSurfactant 2.5% and the rest of preservative water are stirred and dissolved at 80°C, and after cooling, 0.1% vitamin C and 0.03% sodium pyrosulfite are added to prepare uniform and transparent rattan tea extract polymer micelles. The preservative water ingredients include 5% butanediol, 0.5% cinnamaldehyde, 0.5% hexanediol, and 94% deionized water.

[0109] Example 2

[0110] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0111] Based on the weight percentage (the same below), 0.5% of rattan tea extract, Pluracare TMF127 PrillSurfactant 2.5% and the rest of preservative water are stirred and dissolved at 80°C, and after cooling, 0.1% vitamin C and 0.05% sodium pyrosulfite are added to prepare uniform and transparent rattan tea extract polymer micelles. The preservative water ingredients include 5% butanediol, 0.5% cinnamaldehyde, 0.5% hexanediol, and 94% deionized water.

[0112] Example 3

[0113] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0114] Based on the weight percentage (the same below), 0.5% of rattan tea extract, Pluracare TM F127 PrillSurfactant 1.0% and the rest of preservative water are stirred and dissolved at 80°C, and after cooling, 0.1% vitamin C and 0.03% sodium pyrosulfite are added to prepare uniform and transparent rattan tea extract polymer micelles. The preservative water ingredients include 5% butanediol, 0.5% cinnamaldehyde, 0.5% hexanediol, and 94% deionized water.

[0115] Example 4

[0116] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0117] Based on the weight percentage (the same below), 0.5% of rattan tea extract, Pluracare TM F127 PrillSurfactant 1.5% and the rest of preservative water are stirred and dissolved at 80°C, and after cooling, 0.1% vitamin C and 0.03% sodium pyrosulfite are added to prepare uniform and transparent rattan tea extract polymer micelles. The preservative water ingredients include 5% butanediol, 0.5% cinnamaldehyde, 0.5% hexanediol, and 94% deionized water.

[0118] Example 5

[0119] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0120] Based on the weight percentage (the same below), 0.5% of rattan tea extract, Pluracare TMF127 PrillSurfactant 10% and the rest of preservative water are stirred and dissolved at 80°C, and after cooling, 0.1% vitamin C and 0.03% sodium pyrosulfite are added to prepare uniform and transparent rattan tea extract polymer micelles. The preservative water ingredients include 5% butanediol, 0.5% cinnamaldehyde, 0.5% hexanediol, and 94% deionized water.

[0121] Example 6

[0122] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0123] Based on the weight percentage (the same below), 0.5% of rattan tea extract, Pluracare TM F127 PrillSurfactant 2.5% and the rest of preservative water are stirred and dissolved at 80°C, and after cooling, 0.01% vitamin C and 0.01% sodium pyrosulfite are added to prepare uniform and transparent rattan tea extract polymer micelles. The preservative water ingredients include 5% butanediol, 0.5% cinnamaldehyde, 0.5% hexanediol, and 94% deionized water.

[0124] Example 7

[0125] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0126] Based on the weight percentage (the same below), 0.5% of rattan tea extract, Pluracare TM F127 PrillSurfactant 2.5% and the rest of preservative water are stirred and dissolved at 80°C, and after cooling, 1% vitamin C and 0.2% sodium pyrosulfite are added to prepare uniform and transparent rattan tea extract polymer micelles. The preservative water ingredients include 5% butanediol, 0.5% cinnamaldehyde, 0.5% hexanediol, and 94% deionized water.

[0127] Comparative Example 1

[0128] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0129] Based on the weight percentage (the same below), 0.5% of rattan tea extract and the rest of preservative water were stirred and dissolved at 80°C to prepare a uniform and transparent rattan tea extract aqueous solution. The preservative water ingredients include 5% butanediol, 0.5% fennel, 0.5% hexanediol, and 94% deionized water.

[0130] Comparative Example 2

[0131] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0132] Based on the weight percentage (the same below), 0.5% of rattan tea extract, Pluracare TM F127 PrillSurfactant 2.5% and the rest of preservative water are stirred and dissolved at 80°C to prepare uniform and transparent rattan tea extract polymer micelles. The preservative water ingredients include 5% butanediol, 0.5% cinnamaldehyde, 0.5% hexanediol and 94% deionized water.

[0133] Comparative Example 3

[0134] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0135] Based on the weight percentage (the same below), 0.5% of rattan tea extract, 2.5% of HP-β-CD and the rest of preservative water were stirred and dissolved at 80°C to prepare a uniform and transparent rattan tea extract inclusion complex aqueous solution. The preservative water ingredients include 5% butanediol, 0.5% oxadiazine, 0.5% hexanediol and 94% deionized water.

[0136] Comparative Example 4

[0137] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0138] Based on the weight percentage (the same below), 0.5% of rattan tea extract, 2.5% of SOLUBILISANT LRI and the rest of preservative water were stirred and dissolved at 80°C to prepare uniform and transparent rattan tea extract micelles. The preservative water ingredients include 5% butanediol, 0.5% oxadiazine, 0.5% hexanediol and 94% deionized water.

[0139] Comparative Example 5

[0140] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0141] Based on the weight percentage (the same below), 0.5% of rattan tea extract and the rest of preservative water were stirred and dissolved at 80°C, and after cooling, 0.05% sodium pyrosulfite was added to prepare a uniform and transparent rattan tea extract aqueous solution. The preservative water ingredients include 5% butanediol, 0.5% fennel, 0.5% hexanediol, and 94% deionized water.

[0142] Comparative Example 6

[0143] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0144] Based on the weight percentage (the same below), 0.5% of rattan tea extract and the rest of preservative water were stirred and dissolved at 80°C, and after cooling, 0.05% vitamin C was added to prepare a uniform and transparent rattan tea extract aqueous solution. The preservative water ingredients include 5% butanediol, 0.5% fennel, 0.5% hexanediol, and 94% deionized water.

[0145] Comparative Example 7

[0146] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0147] Based on the weight percentage (the same below), 0.5% of rattan tea extract and the rest of preservative water were stirred and dissolved at 80°C, and after cooling, 0.1% vitamin C was added to prepare a uniform and transparent rattan tea extract aqueous solution. The preservative water ingredients include 5% butanediol, 0.5% fennel, 0.5% hexanediol, and 94% deionized water.

[0148] Comparative Example 8

[0149] The rattan tea from the raw material of Agave sphenanthera was refluxed and extracted twice with 10 times hot water, refrigerated overnight, centrifuged and the supernatant was discarded, the precipitate was dissolved with 95% ethanol at a volume of 3 times the weight of the precipitate, the clear liquid was filtered, concentrated, and vacuum dried to obtain the rattan tea extract.

[0150] Based on the weight percentage (the same below), 0.5% of rattan tea extract, Pluracare TMF127 PrillSurfactant 2.5% and the rest of preservative water are stirred and dissolved at 80°C, and after cooling, 0.1% vitamin C is added to prepare uniform and transparent rattan tea extract polymer micelles. The preservative water ingredients include 5% butanediol, 0.5% cinnamaldehyde, 0.5% hexanediol, and 94% deionized water.

[0151] Effect Example

[0152] Effect Example 1. Water Solubility

[0153] The prepared Examples 1-7 and Comparative Examples 1-8 were stored at 25° C. for 4 days. After 4 days, the solution was observed to see if there was precipitation. The results are shown in Table 1 below:

[0154] Table 1

[0155]

[0156]

[0157] It can be seen from the results in Table 1 that Comparative Example 1 (containing only rattan tea) showed a large amount of crystalline precipitates after standing at 25°C for 4 days, and the addition of antioxidants (Comparative Examples 5 and 6) had no effect on improving solubility. Theoretically, HP-β-CD is a derivative of β-CD and has better water solubility and solubilizing ability. However, Comparative Example 3 containing HP-β-CD has poor clarity and powdery precipitates. Theoretically, SOLUBILISANT LRI is widely used to solubilize flavors in cosmetics and has the characteristics of low irritation and strong solubilizing ability. However, Comparative Example 4 containing SOLUBILISANT LRI has granular precipitates. Compared with the above-mentioned solubilizers, Comparative Example 2 (containing Pluracare TM F127 Prill Surfactant) has excellent solubilization effect, clear and transparent appearance, no precipitation, and good stability. TM When the amount of F127 Prill Surfactant is as low as 1.0% (Example 3), it can still effectively solubilize the extract of rattan tea. The results show that the amphiphilic block copolymer Pluracare TM F127 PrillSurfactant has better solubilizing ability than cyclodextrin and small molecule surfactants. TM The water solubility of F127 Prill Surfactant + VC + sodium metabisulfite) is no different from that of Comparative Example 2, indicating that in the presence of antioxidants, Pluracare TMF127 Prill Surfactant still has a strong solubilizing effect.

[0158] Effect Example 2. Stability

[0159] The content of dihydromyricetin in the rattan tea extract was determined by HPLC, with a detection wavelength of 292 nm, and the calculation formula is as follows:

[0160]

[0161] Wherein, ρ is the mass concentration of the analyte in the sample solution obtained from the standard curve, in milligrams per milliliter (mg / mL), V is the fixed volume of the sample, in milliliters (mL), and m is the mass of the sample, in milligrams (mg).

[0162] According to calculation, the content of dihydromyricetin in the rattan tea extracts used in Examples 1-7 and Comparative Examples 1-8 was 72.48%.

[0163] The retention rate of dihydromyricetin in the prepared Examples 1-5 and Comparative Examples 1-8 was calculated after being stored at 60° C. for 7 days and 14 days. The retention rate was calculated as follows:

[0164] The retention rate of dihydromyricetin in the sample after storage for a certain period of time was determined by HPLC, with a detection wavelength of 292 nm and the calculation formula as follows:

[0165]

[0166] In the formula, A n is the peak area of ​​dihydromyricetin in the sample on day n, and A0 is the peak area of ​​dihydromyricetin in the initial sample.

[0167] The calculated results are shown in Table 2 below:

[0168] Table 2

[0169]

[0170]

[0171] At the same time, the samples of Examples 1-5 and Comparative Examples 1-8 were recorded before storage at 60°C (see Figure 1 ), after storage at 60°C for 7 days (see Figure 2 ) and after storage at 60°C for 14 days (see Figure 3 )’s appearance.

[0172] From the above table 2 and Figure 1-3The results show that when placed at 60°C, the color of Comparative Example 1 (containing only rattan tea) darkened significantly, crystalline precipitates appeared, and the content of dihydromyricetin dropped significantly. The retention rate was 55.02% at 7 days and only 37.90% at 14 days. When only the solubilizer was added, Comparative Example 3 (containing HP-β-CD) and Comparative Example 4 (containing SOLUBILISANTLRI) did not improve the discoloration and precipitation problems; Comparative Example 2 (containing Pluracare TM F127 Prill Surfactant) can delay discoloration in the first 14 days and prevent precipitation in the first 7 days. When only antioxidants are added, Comparative Example 5 (containing sodium metabisulfite) can make the rattan tea almost not change color, and the color protection effect of Comparative Example 6 (containing vitamin C) is poor. Both antioxidants show the effect of stabilizing the content of dihydromyricetin. Due to its bad smell and high ionicity, the actual addition amount of sodium metabisulfite in cosmetics often does not exceed 0.05%, and 0.05% sodium metabisulfite has a general protective effect on dihydromyricetin in rattan tea extract. Although vitamin C has a higher dihydromyricetin retention rate at a higher concentration, its color protection effect is poor. For example, the dihydromyricetin content of Comparative Example 8 and Example 2 on the 7th day is almost no loss, but the color of Comparative Example 8 without sodium metabisulfite is darker. It can be seen that the combination of sodium metabisulfite and vitamin C can achieve good results in both color protection and improving the retention rate of dihydromyricetin.

[0173] The retention rates of dihydromyricetin in Examples 1-5 after storage at 60° C. for 14 days all reached over 90%, the discoloration was significantly improved, no precipitation was observed, and the appearance was clear and bright, showing ultra-high stability.

[0174] References

[0175] [1] Xiang Dong, Xiong Wei, Wang Wenqing, et al. Research progress on new technologies and new dosage forms of dihydromyricetin preparations[J]. Chinese Herbal Medicine, 2016, 47(04): 689-694.

[0176] [2] He Guixia, Pei Gang, Li Bin, et al. Study on the stability of dihydromyricetin[J]. Chinese Journal of New Drugs, 2007, (22): 1888-1890.

[0177] [3] Chen Yuqiong, Zhong Mei, Ma Rong. Effects of additives on the quality stability of rattan tea beverages [J]. Journal of Huazhong Agricultural University, 2010, 29(01): 114-119.

Claims

1. A polymer micelle composition comprising the following components: (a) rattan tea extract or dihydromyricetin; (b) an amphiphilic polymer capable of forming polymer micelles; (c) Antioxidants.

2. The polymer micelle composition according to claim 1, wherein the amphiphilic polymer is selected from poloxamer 407, poloxamer 188, poloxamer 184, vitamin E polyethylene glycol succinate or a combination thereof, preferably poloxamer 407.

3. The polymer micelle composition according to claim 2, wherein the poloxamer 407 is Pluracare TM F127 Prill Surfactant.

4. The polymer micelle composition according to any one of claims 1 to 3, wherein the antioxidant is selected from one, a combination of two or more of vitamin C, sodium pyrosulfite, ascorbyl glucoside, vitamin C ethyl ether, gallic acid, propyl gallate, tea polyphenols, butylated hydroxytoluene and epigallocatechin gallate, preferably a combination of vitamin C and sodium pyrosulfite. 5 . The polymer micelle composition according to claim 1 , wherein the composition optionally further comprises water and / or an ingredient having an antibacterial effect.

6. The polymer micelle composition according to claim 5, wherein the component with antibacterial effect is selected from butylene glycol, hexylene glycol, cinnamaldehyde, propylene glycol, pentylene glycol, caprylyl glycol, phenoxyethanol, ethylhexylglycerin or a combination thereof.

7. The polymer micelle composition according to any one of claims 1 to 6, wherein the weight ratio of component (a) to component (b) is 1:1 to 1:40, preferably 1:2 to 1:20; wherein the weight ratio of component (a) to component (c) is 1:20 to 100:1, preferably 5:12 to 25:1; wherein when component (c) is a combination of vitamin C and sodium pyrosulfite, the weight ratio of vitamin C to sodium pyrosulfite is 1:10 to 50:1, preferably 1:1 to 5:

1.

8. The polymer micelle composition according to any one of claims 1 to 7, wherein the concentration of component (a) is 0.01% to 10% by weight, preferably 0.1% to 5%; the concentration of component (b) is greater than its critical micelle concentration and is 0.1% to 50% by weight, preferably 1% to 10%; the concentration of component (c) is 0.001% to 10% by weight, preferably 0.02% to 1.2%; wherein when component (c) is a combination of vitamin C and sodium metabisulfite, the concentration of vitamin C is 0.001% to 10% by weight, preferably 0.01% to 1%, and the concentration of sodium metabisulfite is 0.001% to 10% by weight, preferably 0.01% to 0.2%.

9. The polymer micelle composition according to any one of claims 5-8, wherein when the component with antibacterial effect is a combination of butanediol, hexanediol and cinnamaldehyde, the weight ratio of butanediol to hexanediol is 1:1 to 20:1, preferably 10:1, and the weight ratio of butanediol to cinnamaldehyde is 1:1 to 20:1, preferably 10:

1.

10. The polymer micelle composition according to any one of claims 1 to 9, wherein the content of dihydromyricetin in the Ampelopsis ulmoides extract is 30% to 99% by weight, preferably 60% to 75% by weight.

11. A method for preparing a polymer micelle composition according to any one of claims 1 to 10, the method comprising the following steps: (1) loading component (a) onto an amphiphilic polymer of component (b) to form component (a) fully or partially encapsulated in polymer micelles; (2) Add antioxidants, Wherein step (1) and step (2) can be carried out simultaneously or sequentially; wherein the ratio and content of each component are as defined in any one of claims 1 to 9; optionally, water and / or an ingredient having an antibacterial effect are added simultaneously in step (1).

12. The method according to claim 11, wherein step (1) is performed first and then step (2), and step (1) is performed at a temperature of 60-90°C, preferably 75-85°C, and step (2) is performed at room temperature.

13. The method according to claim 11 or 12, wherein step (1) comprises stirring component (a), component (b) and optional water and / or an ingredient having an antibacterial effect at a temperature of 60-90° C., preferably 75-85° C.; and step (2) comprises adding an antioxidant after cooling the solution obtained in step (1) to room temperature.

14. Use of the polymer micelle composition according to any one of claims 1 to 10 in the preparation of medicines / cosmetics.

15. The use according to claim 14, wherein the medicine / cosmetic has anti-inflammatory, anti-oxidative, whitening, oil-controlling, anti-aging, antibacterial and / or anti-acne effects.

16. A medicine or cosmetic comprising the polymer micelle composition according to any one of claims 1 to 10, wherein the micelle composition accounts for 1% to 60% by weight of the medicine or cosmetic.

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